Synthesis and Biological Evaluation of 2-Substituted Quinoline 6-Carboxamides as Potential mGluR1 Antagonists for the Treatment of Neuropathic Pain
- Synthesis and Biological Evaluation of 2-Substituted Quinoline 6-Carboxamides as Potential mGluR1 Antagonists for the Treatment of Neuropathic Pain
- 김영희; 손지원; 김주현; 백두종; 이용섭; 임은정; 이재균; 배애님; 민선준; 조용서
- glutamate; metabotropic glutamate receptor (mGluR); quinoline; neuropathic pain; spinal nerve ligation (SNL) model
- Issue Date
- Chemical & pharmaceutical bulletin
- VOL 62, NO 6, 508-518
- A series of 2-amino and 2-methoxy quinoline-6-carboxamide derivatives have been synthesized and their metabotropic glutamate receptor type 1 (mGluR1) antagonistic activities were evaluated in a functional cell-based assay. The compound 13c showed the highest potency with IC50 value of 2.16 μM against mGluR1. Finally, in vivo evaluation of 13c in the rat spinal nerve ligation (SNL) model exhibited weak analgesic effects with regard to both mechanical allodynia and cold allodynia.
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